Assay Detail
Functional
CHEMBL1837354
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.13 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1837039 | — | — | 1 | 9.30 |
| CHEMBL1837041 | — | — | 1 | 8.89 |
| CHEMBL1837028 | — | — | 1 | 8.52 |
| CHEMBL1837038 | — | — | 1 | 8.49 |
| CHEMBL1837040 | — | — | 1 | 8.32 |
| CHEMBL1837037 | — | — | 1 | 8.17 |
| CHEMBL1837017 | — | — | 1 | 8.05 |
| CHEMBL419667 | RELCOVAPTAN | 2.0 | 1 | 7.89 |
| CHEMBL1837022 | — | — | 1 | 7.77 |
| CHEMBL1837031 | — | — | 1 | 7.77 |
| CHEMBL1837027 | — | — | 1 | 7.75 |
| CHEMBL1837023 | — | — | 1 | 7.70 |
| CHEMBL1834004 | — | — | 1 | 7.70 |
| CHEMBL1837024 | — | — | 1 | 7.60 |
| CHEMBL1837020 | — | — | 1 | 7.54 |
| CHEMBL1837014 | — | — | 1 | 7.15 |
| CHEMBL1837019 | — | — | 1 | 7.08 |
| CHEMBL1837035 | — | — | 1 | 6.96 |
| CHEMBL1837018 | — | — | 1 | 6.93 |
| CHEMBL1837012 | — | — | 1 | 6.88 |
| CHEMBL1837030 | — | — | 1 | 6.87 |
| CHEMBL1837013 | — | — | 1 | 6.70 |
| CHEMBL1649949 | — | — | 1 | 6.70 |
| CHEMBL1837036 | — | — | 1 | 6.57 |
| CHEMBL1837011 | — | — | 1 | 6.46 |
| CHEMBL1837029 | — | — | 1 | 6.46 |
| CHEMBL1837016 | — | — | 1 | 6.24 |
| CHEMBL1837025 | — | — | 1 | 6.21 |
| CHEMBL1837033 | — | — | 1 | 6.04 |
| CHEMBL1837021 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1837039 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1837041 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1837028 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1837038 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1837040 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1837037 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL1837017 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL419667 | RELCOVAPTAN | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1837022 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1837031 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1837027 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1837023 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1834004 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1837024 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1837020 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1837014 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1837019 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1837035 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1837018 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL1837012 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL1837030 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1837013 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL1649949 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1837036 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL1837011 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL1837029 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL1837016 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1837025 | — | IC50 | = | 609.0 | nM | 6.21 |
| CHEMBL1837033 | — | IC50 | = | 904.0 | nM | 6.04 |
| CHEMBL1837021 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL1837015 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL1837026 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL1837034 | — | IC50 | = | 4480.0 | nM | 5.35 |
| CHEMBL1837032 | — | IC50 | = | 5380.0 | nM | 5.27 |